Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM14392
Substrate
BDBM14391
Meas. Tech.
PDE Enzyme Inhibitor Assays
pH
7.4±n/a
Temperature
303.15±n/a K
IC50
1.3±n/a nM
Comments
cGMP in a 3:1 ratio unlabeled to 3H-labeled at a concentration 1/3Km, such that IC50 = Ki.
Citation
 Allerton, CMBarber, CGBeaumont, KCBrown, DGCole, SMEllis, DLane, CAMaw, GNMount, NMRawson, DJRobinson, CMStreet, SDSummerhill, NW A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. J Med Chem 49:3581-94 (2006) [PubMed]  Article 
Target
Name:
cGMP-specific 3',5'-cyclic phosphodiesterase
Synonyms:
3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase
Type:
Protein
Mol. Mass.:
99975.83
Organism:
Homo sapiens (Human)
Description:
O76074
Residue:
875
Sequence:
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
  
Inhibitor
Name:
BDBM14392
Synonyms:
3-ethyl-5-{5-[(4-ethylpiperazine-1-)sulfonyl]-2-(2-methoxyethoxy)pyridin-3-yl}-2-(pyridin-2-ylmethyl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL209157 | Sildenafil Pyridyl Methyl Analogue 1
Type:
Small organic molecule
Emp. Form.:
C27H34N8O5S
Mol. Mass.:
582.674
SMILES:
CCN1CCN(CC1)S(=O)(=O)c1cnc(OCCOC)c(c1)-c1nc2c(CC)n(Cc3ccccn3)nc2c(=O)[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM14391
Synonyms:
2-amino-9-[(4aR,6R,7R,7aS)-2,7-dihydroxy-2-oxidotetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]-1,9-dihydro-6H-purin-6-one | 9-[(4aR,6R,7R,7aS)-2,7-dihydroxy-2-oxo-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]-2-amino-6,9-dihydro-1H-purin-6-one | GUANOSINE-3 ,5 -MONOPHOSPHATE | US11701371, Compound cGMP | cGMP
Type:
Nucleoside or nucleotide
Emp. Form.:
C10H12N5O7P
Mol. Mass.:
345.2053
SMILES:
Nc1nc2n(cnc2c(=O)[nH]1)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure:
Search PDB for entries with ligand similarity: